Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Ophthalmic disease

Glaucoma

Cannabinoid CB1 receptor (CNR1); CNR2

In vitro and rat studies identified CNR1 and CNR2 agonist prodrugs that could help treat glaucoma. In biochemical studies, phosphonate ester derivatives of the topical CNR1 and CNR2 dual agonist SAD448 showed greater aqueous solubility and chemical stability than the parent compound. In rats receiving topical ocular prodrug delivery, the derivatives showed longer residence in the iris and ciliary body of the eye and lower plasma residence than the parent compound. Next steps could include studying the prodrugs in animal models for glaucoma.
Novartis AG's SAD448 has completed Phase I testing for ocular hypertension.

SciBX 6(26); doi:10.1038/scibx.2013.666
Published online July 11, 2013

Patent and licensing status unavailable

Mainolfi, N. et al. J. Med. Chem.; published online June 5, 2013;
doi:10.1021/jm4004939
Contact: Jeremy M. Sivak, The University of Toronto and the Toronto Western Research Institute, Toronto, Ontario, Canada
e-mail:
jsivak@uhnres.utoronto.ca

Contact: Nello Mainolfi, Novartis Institutes for BioMedical Research, Cambridge, Mass.
e-mail:
nello.mainolfi@novartis.com